Differential effects of 5-fluorouracil on glucose transport and expressions of glucose transporter proteins in gastric cancer cells

Anticancer Drugs. 2010 Mar;21(3):270-6. doi: 10.1097/CAD.0b013e328334562c.

Abstract

Although 5-fluorouracil (5-FU) is a widely used chemotherapeutic agent in the treatment of gastric cancer, the underlying mechanism for 5-FU resistant phenotype, has yet to be elucidated. We hypothesized that the sensitivity of gastric cancer to 5-FU treatment might be related to the rate of glucose transport (GLUT), and investigated the expressions of GLUT1, 2, 3, and 4 in two different gastric cancer cells (SNU-216, moderately differentiated gastric adenocarcinoma; and SNU-668, signet ring cell gastric carcinoma). Immunohistochemistry of GLUT1 and GLUT4 and immunoblot analysis of glycogen synthase kinase 3 were also performed. Hexokinase activity was measured. We found that 5-FU suppressed glucose uptake in SNU-216, while it stimulated GLUT in SNU-668. Further analysis revealed that 5-FU decreased the expression levels of GLUT1, 2, and 4 in SNU-216 cells and increased the expression levels of GLUT1, 2, and 4 in SNU-668 cells. Consistent with GLUT expression levels, immunohistochemistry analysis showed that 5-FU increased GLUT1 and GLUT4 levels in SNU-216 and decreased GLUT1 and GLUT4 levels in SNU-668. We also observed that glycogen synthase kinase 3 activity was decreased in SNU-216 and increased in SNU-668 with 5-FU treatment. No significant difference in hexokinase activities was observed with 5-FU treatment. Taken together, these results suggest that 5-FU exerts differential effects on GLUT depending on gastric cancer cell types, which may indicate a possible explanation, at least in part, for the differing responses to 5-FU chemotherapy in gastric cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimetabolites, Antineoplastic / pharmacology*
  • Biological Transport / drug effects
  • Carcinoma, Signet Ring Cell / metabolism*
  • Cell Line, Tumor
  • Fluorouracil / pharmacology*
  • Glucose / metabolism*
  • Glucose Transport Proteins, Facilitative / agonists
  • Glucose Transport Proteins, Facilitative / antagonists & inhibitors
  • Glucose Transport Proteins, Facilitative / metabolism*
  • Glycogen Synthase Kinase 3 / metabolism
  • Hexokinase / metabolism
  • Humans
  • Stomach Neoplasms / metabolism*

Substances

  • Antimetabolites, Antineoplastic
  • Glucose Transport Proteins, Facilitative
  • Hexokinase
  • Glycogen Synthase Kinase 3
  • Glucose
  • Fluorouracil